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Assay Detail

CHEMBL862702

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
In vitro bone resorption in isolated rabbit osteoclasts
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Cell Type Osteoclast
Confidence 1 — Organism
Curated By Intermediate

Target

Osteoclast (CHEMBL612548)
Type CELL-LINE

Publication

Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Palmer JT, Bryant C, Wang DX, Davis DE, Setti EL, Rydzewski RM, Venkatraman S, Tian ZQ, Burrill LC, Mendonca RV, Springman E, McCarter J, Chung T, Cheung H, Janc JW, McGrath M, Somoza JR, Enriquez P, Yu ZW, Strickley RM, Liu L, Venuti MC, Percival MD, Falgueyret JP, Prasit P, Oballa R, Riendeau D, Young RN, Wesolowski G, Rodan SB, Johnson C, Kimmel DB, Rodan G.
J Med Chem (2005) 48 : 7520 -7534
PubMed 16302794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.64 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200708 1 9.00
CHEMBL200494 1 8.52
CHEMBL198798 1 8.52
CHEMBL200602 1 8.40
CHEMBL426819 1 8.30
CHEMBL200543 1 8.10
CHEMBL435913 1 8.00
CHEMBL200596 1 7.96
CHEMBL414669 1 7.96
CHEMBL200672 1 7.89
CHEMBL200287 1 7.72
CHEMBL370165 1 7.70
CHEMBL200426 1 7.70
CHEMBL199214 1 7.68
CHEMBL198802 1 7.62
CHEMBL381190 1 7.48
CHEMBL200788 1 7.46
CHEMBL199358 1 7.46
CHEMBL199014 1 7.43
CHEMBL199163 1 7.40
CHEMBL200744 1 7.37
CHEMBL200166 1 7.34
CHEMBL200507 1 7.28
CHEMBL372410 1 7.23
CHEMBL200506 1 7.22
CHEMBL200455 1 7.21
CHEMBL371133 1 7.11
CHEMBL199470 1 6.96
CHEMBL381026 1 6.68
CHEMBL197440 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200708 IC50 = 1.0 nM 9.00
CHEMBL200494 IC50 = 3.0 nM 8.52
CHEMBL198798 IC50 = 3.0 nM 8.52
CHEMBL200602 IC50 = 4.0 nM 8.40
CHEMBL426819 IC50 = 5.0 nM 8.30
CHEMBL200543 IC50 = 8.0 nM 8.10
CHEMBL435913 IC50 = 10.0 nM 8.00
CHEMBL200596 IC50 = 11.0 nM 7.96
CHEMBL414669 IC50 = 11.0 nM 7.96
CHEMBL200672 IC50 = 13.0 nM 7.89
CHEMBL200287 IC50 = 19.0 nM 7.72
CHEMBL370165 IC50 = 20.0 nM 7.70
CHEMBL200426 IC50 = 20.0 nM 7.70
CHEMBL199214 IC50 = 21.0 nM 7.68
CHEMBL198802 IC50 = 24.0 nM 7.62
CHEMBL381190 IC50 = 33.0 nM 7.48
CHEMBL200788 IC50 = 35.0 nM 7.46
CHEMBL199358 IC50 = 35.0 nM 7.46
CHEMBL199014 IC50 = 37.0 nM 7.43
CHEMBL199163 IC50 = 40.0 nM 7.40
CHEMBL200744 IC50 = 43.0 nM 7.37
CHEMBL200166 IC50 = 46.0 nM 7.34
CHEMBL200507 IC50 = 52.0 nM 7.28
CHEMBL372410 IC50 = 59.0 nM 7.23
CHEMBL200506 IC50 = 60.0 nM 7.22
CHEMBL200455 IC50 = 61.0 nM 7.21
CHEMBL371133 IC50 = 77.0 nM 7.11
CHEMBL199470 IC50 = 110.0 nM 6.96
CHEMBL381026 IC50 = 210.0 nM 6.68
CHEMBL197440 IC50 = 320.0 nM 6.50